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Trifluridine (NSC 75520) Thymidylate Synthase inhibitor

Cat.No.S1778

Trifluridine (NSC 75520), also known as NSC 529182, Viroptic, Trifluorothymidine, or TFT, is an anti-herpesvirus antiviral agent that acts by interfering with viral DNA replication and is used primarily on the eye.
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Quality Control

Batch: Purity: 99.96%
99.96

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (199.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 59 mg/mL

Ethanol : 59 mg/mL

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 296.2 Formula

C10H11F3N2O5

Storage (From the date of receipt)
CAS No. 70-00-8 Download SDF Storage of Stock Solutions

Synonyms NSC 529182, NSC 75520, Viroptic, Trifluorothymidine, TFT SMILES C1C(C(OC1N2C=C(C(=O)NC2=O)C(F)(F)F)CO)O

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
DNA synthesis
In vitro
Trifluridine (NSC 75520) inhibits proliferations of mouse bone marrow cells and human colorectal carcinoma cells implanted to nude mice dose-dependently. It also inhibits colony formation of bone marrow cells in a concentration-dependent manner. This compound and 2'-deoxy-5-fluorouridine (FdUrd) are incorporated into DNA with different efficiencies due to differences in the substrate specificities of TK1 and DUT, causing abundant FTD incorporation into DNA. FTD-treated cells shows differing nuclear morphologies compared to FdUrd-treated cells. It further inhibits proliferations of mouse bone marrow cells and human colorectal carcinoma cells implanted to nude mice dose-dependently.
In vivo
Trifluridine (NSC 75520) has significantly fewer swabs positive for HSV-1 than the untreated eyes in the infected rabbits. This compound has increased antitumor activity and is incorporated into DNA more effectively than continuously infused Trifluridine in mice. It gradually accumulates in tumor cell DNA, in a TPI-independent manner, and significantly delays tumor growth and prolonged survival in mice, compared to treatment with 5-FU derivatives. Furthermore, it results in significantly lower viral titers, fewer HSV-1-positive eyes/total during the treatment period, lower keratitis scores, fewer eyes with keratitis/total, and a shorter time to resolution of keratitis in the New Zealand rabbit ocular model.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/2539342/
  • [5] https://pubmed.ncbi.nlm.nih.gov/25230742/
  • [6] https://pubmed.ncbi.nlm.nih.gov/9950596/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06197425 RECRUITING
Colon or Upper Rectum Adenocarcinoma
Centre Hospitalier Universitaire Dijon
2026-05-07 PHASE3
NCT07381764 NOT_YET_RECRUITING
Metastatic Colorectal Cancer (CRC)
Gruppo Oncologico Italia Meridionale
2026-03-30 PHASE2
NCT07270991 RECRUITING
Metastatic Oesogastric Adenocarcinoma
Federation Francophone de Cancerologie Digestive
2025-12-15 PHASE3
NCT05719558 RECRUITING
Advanced Solid Tumors
Astellas Pharma Global Development, Inc.
2023-03-13 PHASE1
NCT06856837 RECRUITING
Metastatic Colorectal Cancer
Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest
2025-10-27 PHASE2
NCT07286695 NOT_YET_RECRUITING
Metastatic Colorectal Cancer (CRC); Colorectal Cancer
Cancer Institute and Hospital, Chinese Academy of Medical Sciences
2025-12-31 PHASE2

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